杨志福, 周四元, 杨铁虹, 梅其炳. 间硝苯地平在Beagle犬体内的药代动力学J. 药学学报, 2004, 39(8): 609-612.
引用本文: 杨志福, 周四元, 杨铁虹, 梅其炳. 间硝苯地平在Beagle犬体内的药代动力学J. 药学学报, 2004, 39(8): 609-612.
YANG Zhi-fu, ZHOU Si-yuan, YANG Tie-hong, MEI Qi-bing. Pharmacokinetics of m-nifedipine in Beagle dogsJ. Acta Pharmaceutica Sinica, 2004, 39(8): 609-612.
Citation: YANG Zhi-fu, ZHOU Si-yuan, YANG Tie-hong, MEI Qi-bing. Pharmacokinetics of m-nifedipine in Beagle dogsJ. Acta Pharmaceutica Sinica, 2004, 39(8): 609-612.

间硝苯地平在Beagle犬体内的药代动力学

Pharmacokinetics of m-nifedipine in Beagle dogs

  • 摘要: 目的用反相高效液相色谱法研究间硝苯地平(m-nifedipine,m-Nif)在Beagle犬体内的药代动力学特征。方法正交设计优化色谱分离条件,Beagle犬分别iv给予m-Nif 0.288 mg·kg-1和ig m-Nif 1.152,3.456,10.370 mg·kg-1。用反相高效液相色谱法分析血浆中原型药物浓度,血浆药物浓度-时间数据用3P97药代动力学软件分析。结果Beagle犬iv m-Nif,其体内过程符合二室模型,T1/2β为116.8 min;ig给予m-Nif 后在Beagle犬体内的代谢符合一室模型,其中低剂量(1.152 mg·kg-1)组Cmax为20 μg·L-1T1/2(ke)为147 min;中剂量(3.456 mg·kg-1)组Cmax为36 μg·L-1T1/2(ke) 为122 min;高剂量(10.37 mg·kg-1)组Cmax为69 μg·L-1T1/2(ke)为144 min。结论Beagle犬ig和iv m-Nif 后,血浆中药物消除迅速,口服绝对生物利用度较低。

     

    Abstract: AimTo study the pharmacokinetics of m-nifedipine (m-Nif) in Beagle dogs. Methods The Beagle dogs were divided into two groups. m-Nif was intravenously administered to the Beagle dogs in group 1 at the dose of 0.288 mg·kg-1, and it was orally administered to the Beagle dogs in group 2,3 and 4 at the dose of 1.152, 3.456 and 10.370 mg·kg-1, respectively. m-Nif in plasma was detected by reversed phase high performance liquid chromatography. The pharmacokinetic parameters were calculated by 3P97 software. ResultsWhen m-Nif was intravenously administered, the plasma concentration-time curve was fit to a two-compartment model and T1/2β was 117 min. When m-Nif was orally administered, the plasma concentration-time curve was fit to a one-compartment model. T1/2(ke) and Cmax were 147 min and 20 μg·L-1; at the low dose of 1.152 mg·kg-1. T1/2(ke) was 122 min and Cmax was 36 μg·L-1 at the middle dose of 3.456 mg·kg-1. T1/2(ke)was 144 min and Cmax was 69 μg·L-1 at the high dose of 10.37 mg·kg-1, respectively. ConclusionIt was showed that the speed of elimination of m-Nif was high in Beagle dogs. The absolute bioavailability of m-Nif given orally was very low.

     

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